α1L‐Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man
The α1‐adrenoceptor population mediating contractile responses to noradrenaline (NA) in smooth muscles of the bladder neck from rabbit (RBN) has been characterized by use of quantitative receptor pharmacology. Experiments with several ‘key’ α1‐adrenoceptor antagonists of varying subtype selectivitie...
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| Veröffentlicht in: | British journal of pharmacology 1998-04, Vol.123 (7), p.1359-1366 |
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| creator | Shannon Kava, M. Blue, David R. Vimont, Rachel L. Clarke, David E. Ford, Anthony P. D. W. |
| description | The α1‐adrenoceptor population mediating contractile responses to noradrenaline (NA) in smooth muscles of the bladder neck from rabbit (RBN) has been characterized by use of quantitative receptor pharmacology.
Experiments with several ‘key’ α1‐adrenoceptor antagonists of varying subtype selectivities (RS‐17053, BMY 7378, indoramin, 5‐methylurapidil, prazosin, REC 15/2739, SNAP 5089, terazosin, WB 4101, tamsulosin, (+)‐cyclazosin and RS‐100329) were conducted. Schild regression analyses yielded affinity (mean pKb) estimates of 7.1, 6.2, 8.6, 8.6, 8.4, 9.3, 7.0, 7.4, 8.9, 10.0, 7.1 and 9.3, respectively, although deviations from unit Schild regression slope question the robustness of data for RS‐17053 and SNAP 5089.
The nature of antagonism by these agents and the profile of affinity determinations generated together suggest that a single α1‐adrenoceptor subtype mediates contractile responses of RBN to NA. Additional studies with phenylephrine indicated also an agonist‐independence of this profile. Pharmacologically, this profile was reminiscent of that described as ‘α1L’ ‐adrenoceptor, which has been shown to mediate contractions of several tissues including lower urinary tract (LUT) tissues of man. Furthermore, a similarity was noticed between the ‘α1L’ ‐adrenoceptor described here in RBN and the rabbit and human cloned α1a‐adrenoceptor (based on data from both whole cell radioligand binding at 37°C and [3H]‐inositol phosphates accumulation assays), characterizations of which have been published elsewhere.
In conclusion, the RBN appears to provide a predictive pharmacological assay for the study of NA‐induced smooth muscle contraction in LUT tissues of man.
British Journal of Pharmacology (1998) 123, 1359–1366; doi:10.1038/sj.bjp.0701748 |
| doi_str_mv | 10.1038/sj.bjp.0701748 |
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Experiments with several ‘key’ α1‐adrenoceptor antagonists of varying subtype selectivities (RS‐17053, BMY 7378, indoramin, 5‐methylurapidil, prazosin, REC 15/2739, SNAP 5089, terazosin, WB 4101, tamsulosin, (+)‐cyclazosin and RS‐100329) were conducted. Schild regression analyses yielded affinity (mean pKb) estimates of 7.1, 6.2, 8.6, 8.6, 8.4, 9.3, 7.0, 7.4, 8.9, 10.0, 7.1 and 9.3, respectively, although deviations from unit Schild regression slope question the robustness of data for RS‐17053 and SNAP 5089.
The nature of antagonism by these agents and the profile of affinity determinations generated together suggest that a single α1‐adrenoceptor subtype mediates contractile responses of RBN to NA. Additional studies with phenylephrine indicated also an agonist‐independence of this profile. Pharmacologically, this profile was reminiscent of that described as ‘α1L’ ‐adrenoceptor, which has been shown to mediate contractions of several tissues including lower urinary tract (LUT) tissues of man. Furthermore, a similarity was noticed between the ‘α1L’ ‐adrenoceptor described here in RBN and the rabbit and human cloned α1a‐adrenoceptor (based on data from both whole cell radioligand binding at 37°C and [3H]‐inositol phosphates accumulation assays), characterizations of which have been published elsewhere.
In conclusion, the RBN appears to provide a predictive pharmacological assay for the study of NA‐induced smooth muscle contraction in LUT tissues of man.
British Journal of Pharmacology (1998) 123, 1359–1366; doi:10.1038/sj.bjp.0701748</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1038/sj.bjp.0701748</identifier><identifier>PMID: 9579731</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Lower urinary tract ; prazosin ; α1A‐adrenoceptor ; α1L‐adrenoceptor</subject><ispartof>British journal of pharmacology, 1998-04, Vol.123 (7), p.1359-1366</ispartof><rights>1998 British Pharmacological Society</rights><rights>Copyright 1998, Nature Publishing Group 1998 Nature Publishing Group</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1565303/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1565303/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,1411,1427,27901,27902,45550,45551,46384,46808,53766,53768</link.rule.ids></links><search><creatorcontrib>Shannon Kava, M.</creatorcontrib><creatorcontrib>Blue, David R.</creatorcontrib><creatorcontrib>Vimont, Rachel L.</creatorcontrib><creatorcontrib>Clarke, David E.</creatorcontrib><creatorcontrib>Ford, Anthony P. D. W.</creatorcontrib><title>α1L‐Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man</title><title>British journal of pharmacology</title><description>The α1‐adrenoceptor population mediating contractile responses to noradrenaline (NA) in smooth muscles of the bladder neck from rabbit (RBN) has been characterized by use of quantitative receptor pharmacology.
Experiments with several ‘key’ α1‐adrenoceptor antagonists of varying subtype selectivities (RS‐17053, BMY 7378, indoramin, 5‐methylurapidil, prazosin, REC 15/2739, SNAP 5089, terazosin, WB 4101, tamsulosin, (+)‐cyclazosin and RS‐100329) were conducted. Schild regression analyses yielded affinity (mean pKb) estimates of 7.1, 6.2, 8.6, 8.6, 8.4, 9.3, 7.0, 7.4, 8.9, 10.0, 7.1 and 9.3, respectively, although deviations from unit Schild regression slope question the robustness of data for RS‐17053 and SNAP 5089.
The nature of antagonism by these agents and the profile of affinity determinations generated together suggest that a single α1‐adrenoceptor subtype mediates contractile responses of RBN to NA. Additional studies with phenylephrine indicated also an agonist‐independence of this profile. Pharmacologically, this profile was reminiscent of that described as ‘α1L’ ‐adrenoceptor, which has been shown to mediate contractions of several tissues including lower urinary tract (LUT) tissues of man. Furthermore, a similarity was noticed between the ‘α1L’ ‐adrenoceptor described here in RBN and the rabbit and human cloned α1a‐adrenoceptor (based on data from both whole cell radioligand binding at 37°C and [3H]‐inositol phosphates accumulation assays), characterizations of which have been published elsewhere.
In conclusion, the RBN appears to provide a predictive pharmacological assay for the study of NA‐induced smooth muscle contraction in LUT tissues of man.
British Journal of Pharmacology (1998) 123, 1359–1366; doi:10.1038/sj.bjp.0701748</description><subject>Lower urinary tract</subject><subject>prazosin</subject><subject>α1A‐adrenoceptor</subject><subject>α1L‐adrenoceptor</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><recordid>eNpVkUtOwzAYhC0EgvLYsvYFUuzYjh0WSKXiJVWCBawtP8Ehias4peoObsBVuAiH4CSkBSGx-qUZzad_NAAcYzTGiIiTVI11NR8jjjCnYguMMOVFxojA22CEEOIZxkLsgf2UKoQGk7NdsFsyXnKCR-Dt8wPPvl7fJ7ZzbTRu3scONs4G1YfYwuhhamLsn2CzSKZ20MS275TZmKGFndI69FDXylrXwdaZ51OoYBOtq6EfUHVcDvqiC63qVnAThX1IaeHSGt6o9hDseFUnd_R7D8DD5cX99Dqb3V7dTCezrMoR45nlmnKjKCfEEFJar1XpmSVC-7yg2lPNckOUpbjI8xJxL3hJvfDECVXgnJIDcPbDnS_0UNC4dZFazrvQDK_JqIL877ThST7GF4lZwQgiA4D8AJahdqu_IEZyPYRMlRyGkL9DyPO764JhTr4Bp8CCjg</recordid><startdate>199804</startdate><enddate>199804</enddate><creator>Shannon Kava, M.</creator><creator>Blue, David R.</creator><creator>Vimont, Rachel L.</creator><creator>Clarke, David E.</creator><creator>Ford, Anthony P. D. W.</creator><general>Blackwell Publishing Ltd</general><scope>5PM</scope></search><sort><creationdate>199804</creationdate><title>α1L‐Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man</title><author>Shannon Kava, M. ; Blue, David R. ; Vimont, Rachel L. ; Clarke, David E. ; Ford, Anthony P. D. W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j2057-d7b47ca4733c339dfba9f5d38bf264bf4b52c3ad41622907f8794f8f3e8a61243</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Lower urinary tract</topic><topic>prazosin</topic><topic>α1A‐adrenoceptor</topic><topic>α1L‐adrenoceptor</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shannon Kava, M.</creatorcontrib><creatorcontrib>Blue, David R.</creatorcontrib><creatorcontrib>Vimont, Rachel L.</creatorcontrib><creatorcontrib>Clarke, David E.</creatorcontrib><creatorcontrib>Ford, Anthony P. D. W.</creatorcontrib><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shannon Kava, M.</au><au>Blue, David R.</au><au>Vimont, Rachel L.</au><au>Clarke, David E.</au><au>Ford, Anthony P. D. W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>α1L‐Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man</atitle><jtitle>British journal of pharmacology</jtitle><date>1998-04</date><risdate>1998</risdate><volume>123</volume><issue>7</issue><spage>1359</spage><epage>1366</epage><pages>1359-1366</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><abstract>The α1‐adrenoceptor population mediating contractile responses to noradrenaline (NA) in smooth muscles of the bladder neck from rabbit (RBN) has been characterized by use of quantitative receptor pharmacology.
Experiments with several ‘key’ α1‐adrenoceptor antagonists of varying subtype selectivities (RS‐17053, BMY 7378, indoramin, 5‐methylurapidil, prazosin, REC 15/2739, SNAP 5089, terazosin, WB 4101, tamsulosin, (+)‐cyclazosin and RS‐100329) were conducted. Schild regression analyses yielded affinity (mean pKb) estimates of 7.1, 6.2, 8.6, 8.6, 8.4, 9.3, 7.0, 7.4, 8.9, 10.0, 7.1 and 9.3, respectively, although deviations from unit Schild regression slope question the robustness of data for RS‐17053 and SNAP 5089.
The nature of antagonism by these agents and the profile of affinity determinations generated together suggest that a single α1‐adrenoceptor subtype mediates contractile responses of RBN to NA. Additional studies with phenylephrine indicated also an agonist‐independence of this profile. Pharmacologically, this profile was reminiscent of that described as ‘α1L’ ‐adrenoceptor, which has been shown to mediate contractions of several tissues including lower urinary tract (LUT) tissues of man. Furthermore, a similarity was noticed between the ‘α1L’ ‐adrenoceptor described here in RBN and the rabbit and human cloned α1a‐adrenoceptor (based on data from both whole cell radioligand binding at 37°C and [3H]‐inositol phosphates accumulation assays), characterizations of which have been published elsewhere.
In conclusion, the RBN appears to provide a predictive pharmacological assay for the study of NA‐induced smooth muscle contraction in LUT tissues of man.
British Journal of Pharmacology (1998) 123, 1359–1366; doi:10.1038/sj.bjp.0701748</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>9579731</pmid><doi>10.1038/sj.bjp.0701748</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | British journal of pharmacology, 1998-04, Vol.123 (7), p.1359-1366 |
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| source | Wiley Free Content; Wiley Online Library Journals Frontfile Complete; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Alma/SFX Local Collection |
| subjects | Lower urinary tract prazosin α1A‐adrenoceptor α1L‐adrenoceptor |
| title | α1L‐Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man |
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